|Systematic (IUPAC) name|
|Excretion||75% biliary, 25% renally|
|Mol. mass||459.497 g/mol|
|(what is this?)|
Apixaban (BMS-562247-01, tradename Eliquis) is an anticoagulant for the treatment of venous thromboembolic events. It is a direct factor Xa inhibitor. Apixaban has been available in Europe since May 2012. In the United States, it is undergoing phase III trials for the prevention of venous thromboembolism. An FDA decision on apixaban which was expected on June 28, 2012 was delayed. On August 21, 2014, Pfizer announced that Apixaban was now FDA approved for treatment and secondary prophylaxis of DVT and PE. It is being developed in a joint venture by Pfizer and Bristol-Myers Squibb.
A 2007 trial showed that apixaban was equivalent to enoxaparin/open-label heparin in preventing thrombosis in patients who had undergone a knee replacement. A 2010 trial showed that apixaban was superior to enoxaparin in preventing thrombosis in patients undergoing elective hip replacement surgery, with similar bleeding rates.
A 2011 trial showed that in patients with atrial fibrillation who have failed or are not candidates for vitamin K antagonist therapy, apixaban, as compared with aspirin, reduced the risk of stroke or systemic embolism in patients experiencing atrial fibrillation by more than 50% (from 3.7% per year with aspirin to 1.6% per year with Apixaban). Difference in death rates did not reach statistical significance. A 2011 trial showed that patients receiving apixaban after acute coronary syndrome experienced an increased rate of major bleeding episodes without a significant reduction in recurrent ischemic events. For this reason, the trial was terminated early.
In a head-to-head study of apixaban versus warfarin, apixaban met both its primary endpoint (“noninferiority” to warfarin in preventing strokes) and a key secondary endpoint (superior compared to warfarin in avoiding major bleeding).
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